EP0683792A4 - Lhrh antagonists having modified aminoacyl residues at postions 5 and 6. - Google Patents

Lhrh antagonists having modified aminoacyl residues at postions 5 and 6.

Info

Publication number
EP0683792A4
EP0683792A4 EP94905391A EP94905391A EP0683792A4 EP 0683792 A4 EP0683792 A4 EP 0683792A4 EP 94905391 A EP94905391 A EP 94905391A EP 94905391 A EP94905391 A EP 94905391A EP 0683792 A4 EP0683792 A4 EP 0683792A4
Authority
EP
European Patent Office
Prior art keywords
aminoacyl residues
postions
lhrh antagonists
modified aminoacyl
alkylated
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP94905391A
Other languages
German (de)
French (fr)
Other versions
EP0683792B1 (en
EP0683792A1 (en
Inventor
Fortuna Haviv
Jonathan Greer
Rolf E Swenson
Daryl R Sauer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abbott Laboratories
Original Assignee
Abbott Laboratories
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Abbott Laboratories filed Critical Abbott Laboratories
Publication of EP0683792A1 publication Critical patent/EP0683792A1/en
Publication of EP0683792A4 publication Critical patent/EP0683792A4/en
Application granted granted Critical
Publication of EP0683792B1 publication Critical patent/EP0683792B1/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substimtedamino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or OMEGA -(substitutedamino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.
EP94905391A 1992-12-18 1993-12-14 Lhrh antagonists having modified aminoacyl residues at postions 5 and 6 Expired - Lifetime EP0683792B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US99320292A 1992-12-18 1992-12-18
US993202 1992-12-18
PCT/US1993/012196 WO1994014841A1 (en) 1992-12-18 1993-12-14 Lhrh antagonists having modified aminoacyl residues at postions 5 and 6

Publications (3)

Publication Number Publication Date
EP0683792A1 EP0683792A1 (en) 1995-11-29
EP0683792A4 true EP0683792A4 (en) 1998-11-18
EP0683792B1 EP0683792B1 (en) 2001-09-26

Family

ID=25539225

Family Applications (1)

Application Number Title Priority Date Filing Date
EP94905391A Expired - Lifetime EP0683792B1 (en) 1992-12-18 1993-12-14 Lhrh antagonists having modified aminoacyl residues at postions 5 and 6

Country Status (11)

Country Link
US (1) US5491217A (en)
EP (1) EP0683792B1 (en)
JP (1) JP3568952B2 (en)
AT (1) ATE206136T1 (en)
CA (1) CA2136079A1 (en)
DE (1) DE69330838T2 (en)
DK (1) DK0683792T3 (en)
ES (1) ES2164096T3 (en)
MX (1) MX9308014A (en)
PT (1) PT683792E (en)
WO (1) WO1994014841A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4801577A (en) * 1987-02-05 1989-01-31 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
US5516759A (en) * 1994-12-08 1996-05-14 Tap Holdings Inc. LHRH antagonists having lactam groups at the N-terminus
US5681928A (en) * 1994-12-16 1997-10-28 The Salk Institute For Biological Studies Betides and methods for screening peptides using same
US5843901A (en) * 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
DE19544212A1 (en) * 1995-11-28 1997-06-05 Asta Medica Ag New LH-RH antagonists with improved effects
US5925730A (en) * 1997-04-11 1999-07-20 Ferring Bv GnRH antagonists
MXPA02008870A (en) 2000-03-14 2003-06-24 Zentaris Ag Novel lhrh antagonists, production and use thereof as medicament.
US7098305B2 (en) 2001-09-06 2006-08-29 Ardana Bioscience Limited Sustained release of microcrystalline peptide suspensions
SG173223A1 (en) 2003-04-22 2011-08-29 Ipsen Pharma Sas Peptide vectors
CN101987865B (en) * 2009-07-29 2014-07-30 中国人民解放军军事医学科学院毒物药物研究所 Antagonist of luteinizing hormone releasing hormone (LHRH) containing hydantoin structure

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4317815A (en) * 1979-06-13 1982-03-02 Coy David Howard LH-RH Antagonists
ATE8988T1 (en) * 1980-06-02 1984-09-15 Andrew Victor Schally LH-RH ANTAGONISTS.
US4667014A (en) * 1983-03-07 1987-05-19 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists
US4481190A (en) * 1982-12-21 1984-11-06 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
US4530920A (en) * 1983-11-07 1985-07-23 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH, useful as LHRH agonist
US5073624A (en) * 1985-04-09 1991-12-17 Administrators Of The Tulane Educational Fund Therapeutic decapeptides
US4866160A (en) * 1985-04-09 1989-09-12 The Administrators Of The Tulane Educational Fund Therapeutic decapeptides
US5171835A (en) * 1988-10-21 1992-12-15 The Administrators Of The Tulane Educational Fund LHRH antagonists
US5169932A (en) * 1989-10-30 1992-12-08 The Salk Institute For Biological Studies Gnrh analogs
CN1036343C (en) * 1990-11-10 1997-11-05 天津市计划生育研究所 Synthesis, products and its application for luleinizing hormone releasing hormone and antagonistic znalogue
IL108509A0 (en) * 1993-02-22 1994-05-30 Salk Inst For Biological Studi GnRH antagonist peptides

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
F. HAVIV ET AL.: "The Effect of NMeTyr5 Substitution in Luteinizing Hormone-Releasing Hormone Antagonists", J.MED.CHEM., vol. 36, 1993, pages 928 - 933, XP002075785 *
FLOURET, GEORGE ET AL: "Antiovulatory analogs of LH-RH designed by substituting the nicotinoyl groups of positions 5 and/or 6 of Antide with other heterocyclic acyl groups", PEPT. 1992, PROC. EUR. PEPT. SYMP., 22ND (1993), MEETING DATE 1992, 733-4. EDITOR(S): SCHNEIDER, CONRAD H.;EBERLE, ALEX N. PUBLISHER: ESCOM, LEIDEN, NETH. CODEN: 60LUAN, XP002075786 *
LJUNGQVIST, ANDERS ET AL: "Design, synthesis and biological evaluation of antagonists of LHRH by criteria of potency, safety and solubility", Z. NATURFORSCH., B: CHEM. SCI. (1991), 46(9), 1231-6 CODEN: ZNBSEN;ISSN: 0932-0776, XP002075783 *
RIVIER, JEAN ET AL: "Gonadotropin-releasing hormone antagonists with N.omega.- triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6", J. MED. CHEM. (1992), 35(23), 4270-8 CODEN: JMCMAR;ISSN: 0022-2623, XP002075784 *

Also Published As

Publication number Publication date
WO1994014841A1 (en) 1994-07-07
PT683792E (en) 2002-03-28
DE69330838T2 (en) 2002-04-25
ATE206136T1 (en) 2001-10-15
MX9308014A (en) 1994-08-31
DK0683792T3 (en) 2002-01-14
ES2164096T3 (en) 2002-02-16
JP3568952B2 (en) 2004-09-22
CA2136079A1 (en) 1994-07-07
EP0683792B1 (en) 2001-09-26
US5491217A (en) 1996-02-13
JPH08505611A (en) 1996-06-18
EP0683792A1 (en) 1995-11-29
DE69330838D1 (en) 2001-10-31

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